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New approach in the synthesis of M6G
Authors:Claire TrécantAlain Dlubala  Isabelle RipocheYves Troin
Institution:a Clermont Université, ENSCCF, EA 987, LCHG, BP 10448, F-63000 Clermont-Ferrand, France
b Sanofi-Aventis, Route d’Avignon, 30390 Aramon, France
Abstract:Morphine-6-glucuronide (M6G) is the primarily active metabolite of morphine, produced endogenously by the UGT enzyme, which displays analgesic activity. For this reason, M6G is a promising drug candidate for the treatment of severe pain. We described herein a new, efficient and scalable synthesis of M6G using dimorphinic derivatives. This preparation of M6G could be performed on multigram scale with good yield and high purity.
Keywords:Morphine-6-glucoronide  Analgesic activity  Terephtaloyl chloride  Glycosylation  Multigram scale
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